Abstract
In this work, a new magnetic ligand fishing probe for discovery of DPP-IV inhibitory ligands was developed and it was tested as a proof of concept on the fruit extract of Vaccinium vitis-idaea (lingonberry). The ligands were shown to have appreciable dipeptidyl peptidase IV (DPP-IV) inhibitory activity (IC50: 31.8 μg mL-1).) Inhibition of DPP-IV is a well-known therapeutic approach for management of type 2 diabetes (T2D). DPP-IV was successfully immobilized onto magnetic beads and was shown to retain its catalytic activity and selectivity over a model mixture. A total of four ligands were successfully fished out and identified as cyanidin-3-galactoside (2), cyanidin-3-arabinoside (3), proanthocynidin A (4), and 10-carboxyl-pyranopeonidin 3-O-(6″-O-p-coumaroyl)-glucoside (5) using HPLC/HRMS.
Highlights
Type 2 diabetes (T2D) is a metabolic disorder characterized by impaired function or production of insulin that manifests as a disturbance of glucose homeostasis
The increase of blood glucose levels after food intake leads to secretion of the incretin hormones glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP)
In the present study a new magnetic ligand fishing method was developed for rapid identification of dipeptidyl peptidase IV (DPP-IV) inhibiting ligands from a lingonberry extract
Summary
Type 2 diabetes (T2D) is a metabolic disorder characterized by impaired function or production of insulin that manifests as a disturbance of glucose homeostasis. Once the incretin hormones bind to their receptors, a series of reactions (such as the potentiation of glucose-induced synthesis and secretion of insulin) take place in order to maintain the sugar homeostasis [1, 2]. GLP-1 and GIP are rapidly hydrolyzed by the action of the enzyme DPP-IV, a prolyl peptidase that exists in blood and is ubiquitously expressed on the apical surface of endothelial and epithelial cells. This will constrain the effect of incretins on reducing blood sugar levels [2, 3]. Inhibiting ligands of the alkaline protease DPP-IV are well-recognized as therapeutic agents that can be used for management of hyperglycemia in patients with T2D [4]
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